Pioglitazone alleviates cardiac and vascular remodelling and improves survival in monocrotaline induced pulmonary arterial hypertension

Naunyn Schmiedebergs Arch Pharmacol. 2016 Apr;389(4):369-79. doi: 10.1007/s00210-015-1205-3. Epub 2016 Jan 7.

Abstract

Pulmonary arterial hypertension (PAH) is a fatal disease with limited therapeutic options. Pathophysiological changes comprise obliterative vascular remodelling of small pulmonary arteries, elevated mean pulmonary arterial systolic pressure (PASP) due to elevated resistance of pulmonary vasculature, adverse right ventricular remodelling, and heart failure. Recent findings also indicate a role of increased inflammation and insulin resistance underlying the development of PAH. We hypothesized that treatment of this condition with the peroxisome proliferator-activated receptor-γ (PPARγ) activator pioglitazone, known to regulate the expression of different genes addressing insulin resistance, inflammatory changes, and vascular remodelling, could be a beneficial approach. PAH was induced in adult rats by a single subcutaneous injection of monocrotaline (MCT). Pioglitazone was administered for 2 weeks starting 3 weeks after MCT-injection. At day 35, hemodynamics, organ weights, and -indices were measured. We performed morphological and molecular characterization of the pulmonary vasculature, including analysis of the degree of muscularization, proliferation rates, and medial wall thickness of the small pulmonary arteries. Furthermore, markers of cardiac injury, collagen content, and cardiomyocyte size were analyzed. Survival rates were monitored throughout the experimental period. Pioglitazone treatment improved survival, reduced PASP, muscularization of small pulmonary arteries, and medial wall thickness. Further, MCT-induced right ventricular hypertrophy and fibrosis were attenuated. This was accompanied with reduced cardiac expression of brain natriuretic peptide, as well as decreased cardiomyocyte size. Finally, pulmonary macrophage content and osteopontin gene expression were attenuated. Based on the beneficial impact of pioglitazone, activation of PPARγ might be a promising treatment option in PAH.

Keywords: Monocrotaline; PPAR; Pulmonary hypertension; Rat; Right ventricle.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arterial Pressure / drug effects
  • Cardiovascular Agents / pharmacology*
  • Disease Models, Animal
  • Fibrosis
  • Heart Ventricles / drug effects*
  • Heart Ventricles / metabolism
  • Heart Ventricles / pathology
  • Heart Ventricles / physiopathology
  • Hypertension, Pulmonary / chemically induced
  • Hypertension, Pulmonary / drug therapy*
  • Hypertension, Pulmonary / metabolism
  • Hypertension, Pulmonary / physiopathology
  • Hypertrophy, Right Ventricular / chemically induced
  • Hypertrophy, Right Ventricular / metabolism
  • Hypertrophy, Right Ventricular / physiopathology
  • Hypertrophy, Right Ventricular / prevention & control*
  • Macrophages, Alveolar / drug effects
  • Macrophages, Alveolar / metabolism
  • Male
  • Monocrotaline*
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism
  • Myocytes, Cardiac / pathology
  • Natriuretic Peptide, Brain / metabolism
  • Osteopontin / metabolism
  • PPAR gamma / agonists*
  • PPAR gamma / metabolism
  • Pioglitazone
  • Pulmonary Artery / drug effects*
  • Pulmonary Artery / metabolism
  • Pulmonary Artery / pathology
  • Pulmonary Artery / physiopathology
  • Rats, Sprague-Dawley
  • Thiazolidinediones / pharmacology*
  • Vascular Remodeling / drug effects*
  • Ventricular Function, Right / drug effects
  • Ventricular Remodeling / drug effects*

Substances

  • Cardiovascular Agents
  • PPAR gamma
  • Spp1 protein, rat
  • Thiazolidinediones
  • Osteopontin
  • Natriuretic Peptide, Brain
  • Monocrotaline
  • Pioglitazone